tebipenem and tosufloxacin

In November 2004, "Guidelines for the Management of Respiratory Infectious Diseases in Children in Japan" was published ahead of the rest of the world, by Japanese Society of Pediatric Pulmonology/Japanese Society for Pediatric Infectious Diseases, based on the data on causative organisms in the lower respiratory tract. In its 2011 version, classification of the severity of pneumonia was renewed based on the latest information. As a result, many types of pneumonia in children are now classified as mild or moderate. This means that many patients who might have conventionally required hospital treatment can now be managed on an outpatient basis. The reason for realization of the wider range of outpatient treatment is the availability of two new oral antimicrobial agents, tebipenem pivoxil and tosufloxacin tosilate hydrate, for the treatment of infections in children. Analysis of data on medical expenses shows a decreased rate of hospitalization due to pneumonia year by year after launch of these two drugs, suggesting that these drugs have contributed to wider range of outpatient treatment. This manuscript discusses the effect of tebipenem pivoxil and tosufloxacin tosilate hydrate in the treatment of pneumonia.

Topics: Administration, Oral; Anti-Infective Agents; Carbapenems; Child; Fluoroquinolones; Humans; Naphthyridines; Outpatients; Pneumonia

Topics: Acute Disease; Ampicillin; Anti-Bacterial Agents; beta-Lactam Resistance; Carbapenems; Cephalosporins; Child, Preschool; Drug Resistance, Multiple, Bacterial; Fluoroquinolones; Haemophilus Infections; Haemophilus influenzae; Humans; Infant; Japan; Microbial Sensitivity Tests; Multilocus Sequence Typing; Naphthyridines; Otitis Media; Pneumococcal Vaccines; Quinolones; Streptococcus pneumoniae; Vaccines, Conjugate

Morphological changes in penicillin-resistant Streptococcus pneumoniae (PRSP) and beta-lactamase-nonproducing, ampicillin-resistant Haemophilus influenzae (BLNAR) after exposure to oral antibacterial agents could be observed over time under a phase-contrast microscope. Morphological changes in BLNAR were also observed using a scanning electron microscope. The organisms used in this study were ME19F strain identified as genotypic(g) gPRSP (serotype: 19F) and JPH002 strain identified as gBLNAR (serotype: b). The antibacterial agents used were amoxicillin (AMPC), cefditoren (CDTR), tebipenem (TBPM), and tosufloxacin (TFLX). The concentration of each antibacterial agent to which the bacteria were exposed was set at the blood level one hour after Cmax when administered to children at the usual dose. Bacteriolysis of gPRSP cells started after exposure of only 20minutes to TBPM, and 90% of the cells were lysed within 2 hours. A high bactericidal action of TBPM on gPRSP was supported by these findings. When gBLNAR was exposed to AMPC and TBPM, lysis from spheroplasts and cells with vacuoles were sometimes observed. In contrast, after gBLNAR was exposed to CDTR, lysis occurred after marked filamentation in the cells, but after exposure to TFLX, cells deduced to be killed after mild filamentation without lysis. Time-dependent morphological changes that reflect the differences in bactericidal activity and PBP affinity among beta-lactams provide beneficial information to select antibacterial agents.

Topics: Amoxicillin; Ampicillin Resistance; Anti-Bacterial Agents; Bacteriolysis; beta-Lactamases; Carbapenems; Cephalosporins; Child; Dose-Response Relationship, Drug; Fluoroquinolones; Haemophilus Infections; Haemophilus influenzae; Humans; Microscopy, Phase-Contrast; Naphthyridines; Penicillin Resistance; Pneumococcal Infections; Streptococcus pneumoniae; Time Factors